Ciclesonide aqueous pharmaceutical compositions containing ciclesonide dispersed in an aqueous medium in a form of solid particles are expected to represent a useful drug form for reasons that include 1) it is not necessary to completely dissolve ciclesonide, 2) it can be directly administered to an affected site by spraying and so forth for treatment of local diseases such as those of the nasal mucosa, eyes and epidermis, and 3) they are easier to swallow than tablets or granule and so forth.
When present in an aqueous medium, ciclesonide is resistant to wetting and easily aggregates. The addition of wetting agent such as Polysorbate 80 and powerful stirring and so forth during production have been used in the prior art for the purpose of dispersing drug having such properties in an aqueous medium in a stable state.
Improvement of drug dispersivity of aqueous pharmaceutical compositions containing a drug dispersed in an aqueous medium in form of solid particles by addition of cellulose-based polymer is disclosed in Morishima et al. patent specification of WO99-37286. However, this patent relates to the redispersion of a drug that has settled during storage, and is fundamentally different from the present invention which relates to overcoming drawbacks of the migration of ciclesonide towards bubbles formed by powerful stirring during the production, and the adsorption of ciclesonide to the walls of the production apparatus. Moreover, the concentration of the cellulose-based polymer in the patent specification of Morishima et al. is 0.0001 to 0.003%, and methylcellulose can be used in place of hydroxypropylmethylcellulose for the cellulose-based polymer, while the addition of a nonionic surfactant is also required. It is not easy to deduce the present invention from this patent in which the optimum value of the hydroxypropylmethylcellulose concentration is from 0.01% w/w to 0.5% w/w, and does not require a surfactant.